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Oxazolidinones constitute a novel class of antimicrobials as inhibitors of bacterial ribosomal protein synthesis. In this study, we identified 15 novel oxazolidinone analogs with potent antituberculosis activities. Compounds sy124 and sy125 showed the best activity in vitro (better than that of the linezolid) against various clinically relevant bacterial species, including most Gram-positive bacteria, Mycobacterium spp., and Helicobacter pylori. A cell-based assay indicated that these compounds have a strong ability to kill intracellular pathogens. Our results reveal that the newly identified compounds may be further developed as novel antimicrobial agents.

japanese journal of infectious diseases

An Update on the Structure of Oxazolidinone Analogs and a Comparison with Linezolid in Terms of In Vitro and Intracellular Efficacy against Clinically Relevant Bacterial Species